发明公开
- 专利标题: MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS
- 专利标题(中): 丙型肝炎病毒的大环内酯类抑制剂
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申请号: EP06778069.2申请日: 2006-07-28
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公开(公告)号: EP1919898A1公开(公告)日: 2008-05-14
- 发明人: RABOISSON, Pierre Jean-Marie Bernard , DE KOCK, Herman Augustinus , SIMMEN, Kenneth Alan , JÖNSSON, Carl Erik Daniel , NILSSON, Karl Magnus , ROSENQUIST, Åsa Annica Kristina , SAMUELSSON, Bengt Bertil , ANTONOV, Dmitry , SALVADOR ODÉN, Lourdes , AYESA ALVAREZ, Susana , CLASSON, Björn Olof
- 申请人: Tibotec Pharmaceuticals Ltd. , MEDIVIR AB
- 申请人地址: Eastgate Village Eastgate Little Island Co Cork IE
- 专利权人: Tibotec Pharmaceuticals Ltd.,MEDIVIR AB
- 当前专利权人: Tibotec Pharmaceuticals Ltd.,MEDIVIR AB
- 当前专利权人地址: Eastgate Village Eastgate Little Island Co Cork IE
- 代理机构: Wante, Dirk Paul Maria
- 优先权: EP05107070 20050729; EP06101279 20060203
- 国际公布: WO2007014922 20070208
- 主分类号: C07D401/12
- IPC分类号: C07D401/12 ; C07D403/12 ; C07D245/04 ; A61K31/4523 ; A61P31/14
摘要:
Inhibitors of HCV replication of formula (I) and the N-oxides, salts, or stereoisomers thereof, wherein each dashed line (represented by ------) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is -OR6, -NH-SO2R7; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, or C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 and R5 independently from one another are hydrogen, halo, hydroxy, nitro, cyano, carboxyl, C1-6alkyl, C1-6alkoxy, C1-6alkoxyC1-6alkyl, C1-6alkylcarbonyl, C1-6alkoxy- carbonyl, amino, azido, mercapto, C1-6alkylthio, polyhaloC1-6alkyl, aryl or Het; W is aryl or Het; R6 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; R7 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het; aryl is phenyl or naphthyl, each optionally substituted with 1-3 substituents; Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 - 4 heteroatoms each independently selected from N, O or S, and optionally substituted with 1 -3 substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
公开/授权文献
- EP1919898B1 MACROCYCLIC INHIBITORS OF HEPATITIS C VIRUS 公开/授权日:2011-01-26
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